Tanespimycin (17-allylamino-17-demethoxygeldanamycin, 17-AAG) is a synthetic analogue of geldanamycin, an antibiotic first purified in 1970 from Streptomyces hygroscopicus. Tanespimycin is an Hsp90 inhibitor that has demonstrated the potential to disrupt the activity of multiple oncogenes and cell signaling pathways implicated in tumor growth, including HER2, a key pathway in breast cancer. Tanespimycin was being under development by Kosan Biosciences. It was in phase 3 clinical development with bortezomib for the treatment of multiple myeloma (MM). However, in 2010 the company halted development of tanespimycin, during late-stage clinical trials as a potential treatment for multiple myeloma. While no definitive explanation was given, it has been suggested that Bristol-Myers Squibb halted development over concerns of the financial feasibility of tanespimycin development given the 2014 expiry of the patent on this compound, and the relative expense of manufacture.

FLUCETOREX is a substituted amphetamine with anorectic activity.

Temurtide was developed as an immune adjuvant. Information about the current application of this drug is not available.

Marizomib is a natural beta-lactone produced by the marine bacterium Salinispora tropica. Marizomib has a broad inhibition profile for the 20S proteasome and has been shown to inhibit the CT-L (beta5) CT-T-laspase-like (C-L, beta1) and trypsin-like (T-L, beta2) activities of the 20S proteasome. The drug is being tested in phase II clinical trials for the treatment of Multiple Myeloma and Malignant Glioma and in phase I in patients with Non-small Cell Lung Cancer, Pancreatic Cancer, Melanoma or Lymphoma

The monoterpene perillyl alcohol (POH) is a naturally occurring compound derived from citrus fruits, mint, and herbs. It exhibited chemotherapeutic potential against various malignant tumors in preclinical models and was being tested in clinical trials in patients with refractory advanced cancers. POH was formulated in soft gelatine capsules and orally administered to cancer patients several times a day on a continuous basis. However, such clinical trials in humans yielded disappointing results, also because of the large number of capsules that had to be swallowed caused hard-to-tolerate intestinal side effects, causing many patients to withdraw from treatment due to unrelenting nausea, fatigue, and vomiting. The clinical trials in Brazil have explored intranasal POH delivery as an alternative to circumvent the toxic limitations of oral administration. In these trials, patients with recurrent malignant gliomas were given comparatively small doses of POH via simple inhalation through the nose. Results from these studies showed, that this type of long-term, daily chemotherapy was well tolerated and effective. The precise mechanism of action is still undetermined, but it is known, that perillyl alcohol plays an important role in the process of hepatoma cell invasion and migration via decreasing the activity of Notch signaling pathway and increasing E-cadherin expression regulated by Snail. Another possible mechanism is included inhibition of Na/K-ATPase (NKA). The NKA α1 subunit is known to be superexpresses in glioblastoma cells (GBM) and POH acts in signaling cascades associated with NKA can control cell proliferation and/or cellular death.

Rabusertib is a Chk1 kinase inhibitor which was developed by ICOS for the treatment of cancer. The drug was tested in phase II of clinical trials for pancreatic cancer and non small cell lung carcinoma, but its development was discontinued. Now the drug is undergoing phase I trial in Japanese patients with solid tumors.

Intiquinatine is a quinolone derivative patented by Wayne State University as antineoplastic agent. Intiquinatine exhibited efficacy against early stage mammary cancer (Mam-17/Adr) and showed none of the neuromuscular toxicity.

Icoduline (previously known as CBS-113 A) is a dual inhibitor of 5-lipoxygenase and cyclo-oxygenase with anti-inflammatory properties. This drug was potentially useful in ophthalmology and as an alternative to glucocorticoids. In addition, icoduline was useful to treat skin disorders. The drug participated in the clinical trial for eye disorders in France; however, this study was discontinued.

Nanafrocin (nanaomycin A) belongs to the class of quinone antibiotics isolated from a strain OS-3966 of Streptomyces rosa var. notoensis. Nanafrocin (nanaomycin A) mode of action is dependent on its reduction by the respiratory chain-linked NADH or flavin dehydrogenase of the organism. The reduced form of nanafrocin (nanaomycin A) is quickly auto-oxidized by molecular oxygen producing singlet molecular oxygen (O2−). The ability to produce O2− is related to the antimicrobial activity of nanafrocin (nanaomycin A).

Naminterol [VAL 479], a phenethanolamine derivative, is a β2 adrenoceptor agonist with bronchodilatory properties. The compound was undergoing phase II clinical trials for asthma in Italy.